Clinical Pharmacology of Dilevalol (I). Comparison of the Pharmacokinetic and Pharmacodynamic Properties of Dilevalol and Labetalol after a Single Oral Administration in Healthy Subjects

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Abstract
Dilevalol (25 mg → 50 mg → 100 mg) or labetalol (100 mg) was given orally in six healthy subjects. The study was carried out on four occasions with a week interval. Blood samples for plasma drug concentrations were taken for a 24‐hour post‐drug period. Blood pressure (BP) as well as heart rate (HR) at supine position, during 50° tilting and during a submaximal exercise were measured after each treatment. The mean maximum plasma concentration (Cmax) as well as the mean area under the plasma concentration‐time curve (AUC) increased in a dose‐dependent manner after dilevalol. These parameters after dilevalol 100 mg were significantly lower than after labetalol 100 mg. No significant differences were observed in the time to maximum concentration (tmax), the distribution half‐life (t1/2α) or the elimination half‐life (t1/2β) between dilevalol and labetalol. There were no significant differences in BP at supine position or during 50° tilting among the dosages. Postural changes in HR during 50° tilting was significantly smaller after dilevalol 100 mg than following labetalol 100 mg. The suppressing effect of dilevalol 100 mg on an increase in HR during a submaximal exercise was significantly greater than during labetalol 100 mg. These data indicate that although plasma drug concentrations are lower after dilevalol than following labetalol, the β‐blocking activity of dilevalol is more potent than labetalol.